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    2-[(Amino)-aryl-methylene]-benzo[b]thiophen-3(2H)-ones
    4.
    发明授权
    2-[(Amino)-aryl-methylene]-benzo[b]thiophen-3(2H)-ones 失效
    2 - [（氨基） - 芳基 - 亚甲基] - 苯并[b]噻吩-3（2H） - 酮

    公开(公告)号：US4288437A

    公开(公告)日：1981-09-08

    申请号：US173173

    申请日：1980-07-28

    申请人： Wolfhard Engel ,  Gunter Trummlitz ,  Ernst Seeger ,  Joachim Kahling

    发明人： Wolfhard Engel ,  Gunter Trummlitz ,  Ernst Seeger ,  Joachim Kahling

    IPC分类号： A61K31/38 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P25/08 ,  C07D333/62 ,  C07D333/64 ,  C07D409/06

    CPC分类号： C07D333/62 ,  C07D333/64

    摘要： Compounds of the formula ##STR1## wherein Ar is phenyl; mono- or di-substituted phenyl, where the substituents are one to two halogens, one to two alkyls of 1 to 3 carbon atoms, or one amino, nitro, cyano or trifluoromethyl; or pyridinyl;R is hydrogen, chlorine, methyl or methoxy;R.sub.1 is hydrogen or methyl;R.sub.2 is hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, methyl-(cycloalkyl of 3 to 8 carbon atoms) or --A--R.sub.4,where A is alkylene of 2 to 3 carbon atoms, and R.sub.4 is hydroxyl, methylamino, dimethylamino, N-methyl-ethylamino, diethylamino, pyrrolidino, piperidino, hexamethyleneimino, morpholino or 4-methyl-1-piperazinyl; orR.sub.1 and R.sub.2, together with each other and the nitrogen atom to which they are attached, form a 4- to 7-membered, saturated or mono-unsaturated, unsubstituted or substituted heterocycle which may contain nitrogen, oxygen, sulfur, sulfinyl or sulfonyl as additional ring members, where the substituents are alkyls of 1 to 3 carbon atoms.The compounds are useful as anticonvulsants.

    摘要翻译： 其中Ar是苯基的式IMAMA的化合物; 单取代或二取代的苯基，其中取代基是一至两个卤素，一至二个碳原子数为1至2个的烷基，或一个氨基，硝基，氰基或三氟甲基; 或吡啶基; R是氢，氯，甲基或甲氧基; R1是氢或甲基; R2是氢，1至6个碳原子的烷基，2至6个碳原子的烯基，2至6个碳原子的炔基，3至8个碳原子的环烷基，甲基 - 3至8个碳原子的环烷基或-A -R4，其中A为2至3个碳原子的亚烷基，R4为羟基，甲基氨基，二甲基氨基，N-甲基 - 乙基氨基，二乙基氨基，吡咯烷子基，哌啶子基，六亚甲基亚氨基，吗啉代或4-甲基-1-哌嗪基; 或R 1和R 2彼此连接并与它们相连的氮原子形成可含有氮，氧，硫，亚磺酰基或磺酰基的4-至7-元饱和或单不饱和的未被取代或取代的杂环 作为另外的环成员，其中取代基是1至3个碳原子的烷基。 该化合物可用作抗惊厥药。

    Pharmaceutical compositions containing a 1-phenyl-2,2,4,4-C.sub.1 -C.sub.2 alkyl-3-[4-phenyl of pyridyl)-piperazino]-cyclobutanol-(1) and method of use
    6.
    发明授权
    Pharmaceutical compositions containing a 1-phenyl-2,2,4,4-C.sub.1 -C.sub.2 alkyl-3-[4-phenyl of pyridyl)-piperazino]-cyclobutanol-(1) and method of use 失效
    含有1-苯基-2,2,4,4-C（HD 1 {B -C {HD 2 {B烷基-3- {8-吡啶基]苯基） - 哌嗪基{9-环丁醇 - （1 ）和使用方法

    公开(公告)号：US3992536A

    公开(公告)日：1976-11-16

    申请号：US641337

    申请日：1975-12-16

    申请人： Manfred Kleemann ,  Joachim Kahling ,  Gerhart Griss ,  Rudolf Hurnaus

    发明人： Manfred Kleemann ,  Joachim Kahling ,  Gerhart Griss ,  Rudolf Hurnaus

    IPC分类号： A61K31/495

    CPC分类号： A61K31/495 ,  Y10S514/906

    摘要： Pharmaceutical dosage unit compositions containing as an active ingredient a compound of the formula ##SPC1##WhereinR.sub.1 to R.sub.3, which may be the same or different, represent hydrogen atoms, halogen atoms, hydroxy, trifluoromethyl, benzyloxy, acyloxy groups, alkyl groups with 1 to 6 carbon atoms, alkoxy groups with 1 to 3 carbon atoms, phenyl, cyclohexyl, or 2 of the radicals R.sub.1 to R.sub.3 together represents a methylenedioxy group,R.sub.4 represents a hydrogen atom or an alkyl group with 1 or 2 carbon atoms,R.sub.5 represents a hydrogen atom or an alkyl group with 1 to 3 carbon atoms andR.sub.6 represents a phenyl group, which may be mono- or disubstituted by halogen atoms, trifluoromethyl, hydroxy, nitro, amino, benzyloxy, acyloxy groups, alkyl groups with 1 to 3 carbon atoms, alkoxy groups with 1 to 3 carbon atoms or alkylthio groups with 1 to 3 carbon atoms; or a pyridyl group, optionally substituted by a halogen atom, a hydroxy, nitro, amino, benzyloxy, acyloxy, carboxy group, a carbaloxy group with 1 to 3 carbon atoms in the alkoxy, an alkyl group with 1 to 3 carbon atoms or an alkoxy group with 1 to 3 carbon atoms,Or a salt thereof with a physiologically compatible inorganic or organic acid or base; and a method of using the same as sedatives and muscle relaxants.

    摘要翻译： 含有式+ q，10的化合物作为活性成分的药物剂量单位组合物可以相同或不同，表示氢原子，卤素原子，羟基，三氟甲基，苄氧基，酰氧基，烷基与 1至6个碳原子，具有1至3个碳原子的烷氧基，基团R 1至R 3的苯基，环己基或2一起表示亚甲二氧基，R 4表示氢原子或具有1或2个碳原子的烷基，R 5 表示氢原子或具有1至3个碳原子的烷基，R 6表示可被卤素原子，三氟甲基，羟基，硝基，氨基，苄氧基，酰氧基单 - 或二取代的苯基， 3个碳原子，1〜3个碳原子的烷氧基或1〜3个碳原子的烷硫基; 或任选被卤素原子取代的吡啶基，羟基，硝基，氨基，苄氧基，酰氧基，羧基，烷氧基中具有1至3个碳原子的碳酰氧基，具有1至3个碳原子的烷基或 具有1至3个碳原子的烷氧基，或其与生理上相容的无机或有机酸或碱的盐; 以及将其用作SEDATIVES和MUSCLE RELAXANTS的方法。

    Amino-benzoic acid amides
    7.
    发明授权
    Amino-benzoic acid amides 失效
    氨基 - 苯甲酸酰胺

    公开(公告)号：US4093734A

    公开(公告)日：1978-06-06

    申请号：US734818

    申请日：1976-10-22

    申请人： Gerd Kruger ,  Johannes Keck ,  Klaus Reinhold Noll ,  Helmut Pieper ,  Harald Ziegler ,  Helmut Ballhause ,  Joachim Kahling

    发明人： Gerd Kruger ,  Johannes Keck ,  Klaus Reinhold Noll ,  Helmut Pieper ,  Harald Ziegler ,  Helmut Ballhause ,  Joachim Kahling

    IPC分类号： C07D295/12 ,  A61K31/165 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/535 ,  A61K31/5375 ,  A61P1/04 ,  A61P1/08 ,  A61P25/24 ,  A61P25/26 ,  C07C237/30 ,  C07D207/09 ,  C07D211/26 ,  C07D211/56 ,  C07D211/58 ,  C07D213/40 ,  C07D213/75 ,  C07D233/30 ,  C07D295/13 ,  C07D453/02 ,  C07D207/44

    CPC分类号： C07D213/40 ,  C07D207/09 ,  C07D211/26 ,  C07D211/56 ,  C07D233/30 ,  C07D295/13 ,  C07D453/02

    摘要： Compounds of the formula ##STR1## wherein (A) WHEN THE AMINO-SUBSTITUENT IS IN THE P-POSITION WITH RESPECT TO THE CARBONYL GROUP,R.sub.1 is chlorine in the o-position with respect to the carbonyl group,R.sub.2 is hydrogen, andR.sub.3 is ethylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, N-methyl-cyclohexylamino, benzylamino or 1-ethyl-pyrrolidyl-(2)-aminomethyl, or(b) when the amino-substituent is in the o--, m-- or p-position with respect to the carbonyl group,R.sub.1 is hydrogen, chlorine or bromine,R.sub.2 is trifluoromethyl, nitro or, when R.sub.4 is 1-(alkyl of 1 to 3 carbon atoms)-pyrrolidyl or 1-(alkyl of 1 to 3 carbon atoms)-piperidyl, also fluorine, chlorine, bromine or methyl,R.sub.3 is (alkyl of 1 to 5 carbon atoms)-amino, (cycloalkyl of 3 to 7 carbon atoms)-amino, benzylamino, quinuclidinyl-amino or --NH--(CH.sub.2).sub.n --R.sub.4where R.sub.4 is pyridyl, 1-(alkyl of 1 to 3 carbon atoms)-pyrrolidyl, 1-(alkyl of 1 to 3 carbon atoms)-piperidyl or, when n is 2 or 3, also imidazolonyl, pyrrolidino, piperidino or morpholino, andn is 0, 1, 2 or 3,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anxiolytics, anticonvulsives, antiemetics and antiulcerogenics.

    摘要翻译： 式（A）的化合物其中（A）当氨基取代基位于与碳组相对位置时，R 1为相对于羰基的o位置的氯，R 2为氢，R 3为 是乙基氨基，环戊基氨基，环己基氨基，环庚基氨基，N-甲基 - 环己基氨基，苄基氨基或1-乙基 - 吡咯烷基 - （2） - 氨基甲基，或（B）当氨基取代基位于O-， 对于羰基，R1是氢，氯或溴，R2是三氟甲基，硝基，或当R4是1-（1至3个碳原子的烷基） - 吡咯烷基或1-（1至3个碳原子的烷基）时， - 哌啶基，氟，氯，溴或甲基，R3是（碳原子数1〜5的烷基） - 氨基，（3〜7个碳原子的环烷基） - 氨基，苄基氨基，奎宁环基 - 氨基或-NH-（CH2） n-R4，其中R4是吡啶基，1-（1至3个碳原子的烷基） - 吡咯烷基，1-（1至3个碳原子的烷基） - 哌啶基，或当n是2或3时，也是咪唑啉基，吡咯烷子基，哌啶子基 或mor pholino和N IS 0,1,2或3，以及非毒性，药理学上可接受的酸添加量; 化合物作为它们的有效的有用的ANXIOLYTICS，ANTICONVULSIVES，抗原和抗生素。

    1-Phenyl-2,2,4,4-C.sub.1 -C.sub.2 alkyl-3-[4-(phenyl or pyridyl)-piperazino]-cyclobutanols-(1)
    8.
    发明授权
    1-Phenyl-2,2,4,4-C.sub.1 -C.sub.2 alkyl-3-[4-(phenyl or pyridyl)-piperazino]-cyclobutanols-(1) 失效
    1-苯基-2,2,4,4-C（HD 1 {B -C {HD 2 {B烷基-3- {8 4-（苯基或吡啶基） - 哌嗪基{9-环丁烷醇 - （1）

    公开(公告)号：US3931185A

    公开(公告)日：1976-01-06

    申请号：US413233

    申请日：1973-11-06

    申请人： Manfred Kleemann ,  Joachim Kahling ,  Gerhart Griss ,  Rudolf Hurnaus

    发明人： Manfred Kleemann ,  Joachim Kahling ,  Gerhart Griss ,  Rudolf Hurnaus

    IPC分类号： C07D295/08 ,  A61K31/495 ,  A61K31/496 ,  C07D213/74 ,  C07D213/79 ,  C07D295/00 ,  C07D295/04 ,  C07D295/096 ,  C07D295/135 ,  C07D405/08 ,  C07D295/12

    CPC分类号： C07D295/096 ,  A61K31/495 ,  C07D295/135 ,  Y10S514/906

    摘要： This invention relates to cyclobutane derivatives having the formula ##SPC1##Wherein R.sub.1 to R.sub.3, which may be the same or different, represent hydrogen atoms, halogen atoms, hydroxy, trifluoromethyl, benzyloxy, acyloxy groups, alkyl groups with 1 to 6 carbon atoms, alkoxy groups with 1 to 3 carbon atoms, phenyl, cyclohexyl, or 2 of the radicals R.sub.1 to R.sub.3 together represents a methylenedioxy group,R.sub.4 represents a hydrogen atom or an alkyl group with 1 or 2 carbon atoms,R.sub.5 represents a hydrogen atom or an alkyl group with 1 to 3 carbon atoms andR.sub.6 represents a phenyl group, which may be mono- or disubstituted by halogen atoms, trifluoromethyl, hydroxy, nitro, amino, benzyloxy, acyloxy groups, alkyl groups with 1 to 3 carbon atoms, alkoxy groups with 1 to 3 carbon atoms or alkylthio groups with 1 to 3 carbon atoms; or a pyridyl group, optionally substituted by a halogen atom, a hydroxy, nitro, amino, benzyloxy, acyloxy, carboxy group, a carbalkoxy group with 1 to 3 carbon atoms in the alkoxy, an alkyl group with 1 to 3 carbon atoms or an alkoxy group with 1 to 3 carbon atoms;To salts thereof with physiologically compatible inorganic or organic acids or bases as well as to processes for their preparation.The cyclobutane compounds of the above general formula show valuable pharmacological properties, especially a sedative and muscle relaxing activity.

    摘要翻译： 本发明涉及具有式WHEREIN R 1至R 3的环丁烷衍生物，其可以相同或不同，表示氢原子，卤素原子，羟基，三氟甲基，苄氧基，酰氧基，具有1-6个碳原子的烷基， 1至3个碳原子，基团R 1至R 3的苯基，环己基或2一起表示亚甲二氧基，R 4表示氢原子或具有1或2个碳原子的烷基，R 5表示氢原子或 1至3个碳原子，R 6表示可被卤素原子，三氟甲基，羟基，硝基，氨基，苄氧基，酰氧基，具有1至3个碳原子的烷基，1至3个碳原子的烷基， 3个碳原子或1〜3个碳原子的烷硫基; 或任选被卤素原子取代的吡啶基，羟基，硝基，氨基，苄氧基，酰氧基，羧基，烷氧基中具有1至3个碳原子的烷氧基，具有1至3个碳原子的烷基或 具有1至3个碳原子的烷氧基; 与生理学兼容的有机酸或有机酸或基础同样适用于其制备方法。